HRP20171275T1 - Derivati 2.2-difluoropropionamida bardoksolon metila, polimorfni oblici i postupci njihove upotrebe - Google Patents

Derivati 2.2-difluoropropionamida bardoksolon metila, polimorfni oblici i postupci njihove upotrebe Download PDF

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HRP20171275T1
HRP20171275T1 HRP20171275TT HRP20171275T HRP20171275T1 HR P20171275 T1 HRP20171275 T1 HR P20171275T1 HR P20171275T T HRP20171275T T HR P20171275TT HR P20171275 T HRP20171275 T HR P20171275T HR P20171275 T1 HRP20171275 T1 HR P20171275T1
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polymorphic form
compound
pharmaceutical preparation
use according
condition
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Eric Anderson
Andrea Decker
Xiaofeng Liu
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Reata Pharmaceuticals, Inc.
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    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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Claims (28)

1. Spoj s formulom: [image] ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, naznačen time da je spoj s formulom: [image]
3. Polimorfni oblik spoja u skladu sa zahtjevom 1 ili 2, naznačen time da polimorfni oblik ima uzorak rendgenske difrakcije praha (CuKα) koji obuhvaća halo vršak kod oko 14 °2θ; ili pri čemu polimorfni oblik je solvat koji ima uzorak rendgenske difrakcije praha (CuKα) koji obuhvaća vrške kod oko 5.6, 7.0, 10.6, 12.7, i 14.6 °2θ; ili pri čemu polimorfni oblik je solvat koji ima uzorak rendgenske difrakcije praha (CuKα) koji obuhvaća vrške kod oko 7.0, 7.8, 8.6, 11.9, 13.9 (dvostruki vršak), 14.2, i 16.0 °2θ; ili pri čemu polimorfni oblik je acetonitril hemisolvat koji ima uzorak rendgenske difrakcije praha (CuKα) koji obuhvaća vrške kod oko 7.5, 11.4, 15.6, i 16.6 °2θ; ili pri čemu polimorfni oblik je solvat koji ima uzorak rendgenske difrakcije praha (CuKα) koji obuhvaća vrške kod oko 6.8, 9.3, 9.5, 10.5, 13.6, i 15.6 °2θ.
4. Spoj prema zahtjevu 1 ili 2 ili polimorfni oblik prema zahtjevu 3 naznačen time da je za uporabu kao lijek.
5. Farmaceutski pripravak naznačen time da sadrži: aktivni sastojak koji se sastoji od spoja prema zahtjevu 1 ili 2 ili polimorfnog oblika prema zahtjevu 3, te farmaceutski prihvatljiv nosač.
6. Farmaceutski pripravak prema zahtjevu 5, naznačen time da je farmaceutski pripravak formuliran za davanje: oralno, intraadipozno, intraarterijalno, intraartikularno, intrakranijalno, intradermalno, intralezionalno, intramuskularno, intranazalno, intraokularno, intraperikardijalno, intraperitonealno, intrapleuralno, intraprostatski, intrarektalno, intratekalno, intratrahealno, intratumoralno, intralumbalno, intravaginalno, intravenozno, intravezikularno, intravitralno, liposomalno, lokalno, mukozno, parenteralno, rektalno, pod konjunktivu, subkutano, sublingvalno, topikalno, transbukalno, transdermalno, vaginalno, u kremama, u pripravcima lipida, pomoću katetera, putem ispiranja, putem kontinuirane infuzije, infuzijom, inhalacijom, injekcijom, lokalnim davanjem, ili putem lokalizirane perfuzije.
7. Farmaceutski pripravak prema zahtjevu 6, naznačen time da je farmaceutski pripravak formuliran kao tvrda ili meka kapsula, tableta, sirup, suspenzija, emulzija, otopina, čvrsta disperzija, wafer, ili eliksir.
8. Farmaceutski pripravak prema zahtjevu 5 ili 6, naznačen time da je farmaceutski pripravak formuliran za topikalnu primjenu u obliku odabranom od losiona, kreme, gela, ulja, masti, melema, emulzije, otopine, te suspenzije.
9. Farmaceutski pripravak prema bilo kojem od zahtjeva 5 do 8, naznačen time da je količina aktivnog sastojka od 0.01% do 5 masenih %.
10. Spoj prema zahtjevu 1 ili 2 ili polimorfni oblik prema zahtjevu 3 ili farmaceutski pripravak prema bilo kojem od zahtjeva 5 do 9 naznačen time da je za upotrebu za liječenje ili sprječavanje stanja povezanog s upalom ili oksidativnim stresom.
11. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 10, naznačen time da stanje je kožna bolest ili poremećaj, sepsa, dermatitis, osteoartritis, rak, upala, autoimuna bolest, upalna bolest crijeva, komplikacija od lokaliziranog ili cjelokupnog izlaganja ionizirajućem zračenju, mukozitis, akutno ili kronično zatajenje organa, bolest jetre, pankreatitis, poremećaj oka, plućna bolest, ili dijabetes.
12. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je kožna bolest ili poremećaj koji se bira od dermatitisa, toplinskih ili kemijskih opeklina, kronične rane, akni, alopecije, drugih poremećaja folikula kose, bulozne epidermolize, opeklina od sunca, komplikacija opeklina od sunca, poremećaja pigmentacije kože, stanja kože povezanog sa starenjem, rana nakon operacije, ožiljka od ozljede kože ili opeklina, psorijaze, dermatološke manifestacija autoimune bolesti ili bolesti presatka protiv domaćina, raka kože, te poremećaja koji obuhvaćaju hiperproliferaciju stanica kože.
13. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je dermatitis, koji je alergijski dermatitis, atopijski dermatitis, dermatitis zbog izloženosti kemikalijama, ili dermatitis izazvan zračenjem.
14. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je autoimuna bolest odabrana od reumatoidnog artritisa, lupusa, Crohnove bolesti, te psorijaze.
15. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je bolest jetre odabrana od bolesti masne jetre i hepatitisa.
16. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je poremećaj oka odabran od uveitisa, makularne degeneracije, glaukoma, dijabetičkog makularnog edema, blefaritisa, dijabetičke retinopatije, bolesti ili poremećaja endotela rožnice, postoperativna upala, sindrom suhog oka, alergijski konjunktivitis, te oblik konjunktivitis.
17. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je plućna bolest odabrana od upale pluća, plućne fibroze, KOPB, astme, cistične fibroze, te idiopatske plućne fibroze.
18. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je mukozitis koji proizlazi iz terapije zračenjem ili kemoterapije.
19. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je rak izabran iz karcinoma, sarkoma, limfoma, leukemije, melanoma, mezotelioma, multiplog mijeloma, i seminoma.
20. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 19, naznačen time da stanje je melanom.
21. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 11, naznačen time da stanje je rak, i rak je rak mjehura, krvi, kostiju, mozga, dojke, središnjeg živčanog sustava, grlića maternice, debelog crijeva, endometrija, jednjaka, žučnog mjehura, genitalija, genitourinarnog trakta, glave, bubrega, grkljana, jetre, pluća, mišićnog tkiva, vrata, oralne ili nosne sluznice, jajnika, gušterače, prostate, kože, slezene, tankog crijeva, debelog crijeva, želuca, testisa ili štitnjače.
22. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 21, naznačen time da stanje je rak pluća.
23. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 10 do 22, naznačen time da se spoj, polimorfni oblik, ili farmaceutski pripravak primjenjuje i prije i poslije nakon što je subjekt liječen zračenjem ili kemoterapijom.
24. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 23, naznačen time da liječenje smanjuje nuspojavu terapije zračenjem ili kemoterapijom.
25. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 24, naznačen time da nuspojava je mukozitis i dermatitis.
26. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 19 do 22, naznačen time da se spoj, polimorfni oblik ili farmaceutski pripravak primjenjuje u kombinaciji s imunoterapijom.
27. Spoj, polimorfni oblik ili farmaceutski pripravak za upotrebu prema zahtjevu 26, naznačen time da imunoterapija je protutijelo koje cilja na rak.
28. Spoj prema zahtjevu 1 ili 2 ili polimorfni oblik prema zahtjevu 3 ili farmaceutski pripravak prema bilo kojem od zahtjeva 5 do 9 naznačen time da je za upotrebu za liječenje ili prevenciju neurodegenerativne bolesti.
HRP20171275TT 2012-04-27 2013-04-24 Derivati 2.2-difluoropropionamida bardoksolon metila, polimorfni oblici i postupci njihove upotrebe HRP20171275T1 (hr)

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US201261687669P 2012-04-27 2012-04-27
US201361775288P 2013-03-08 2013-03-08
US201361780444P 2013-03-13 2013-03-13
PCT/US2013/038064 WO2013163344A1 (en) 2012-04-27 2013-04-24 2.2-difluoropropionamide derivatives of bardoxolone methyl, polymorphic forms and methods of use thereof
EP13720708.0A EP2841445B1 (en) 2012-04-27 2013-04-24 2.2-difluoropropionamide derivatives of bardoxolone methyl, polymorphic forms and methods of use thereof

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